Assay Detail
Binding
CHEMBL762825
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Inhibitory concentration against human phosphodiesterase 5 (PDE5) enzyme
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 8.22 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26396 | — | — | 1 | 9.52 |
| CHEMBL282709 | — | — | 1 | 9.21 |
| CHEMBL286723 | — | — | 1 | 9.05 |
| CHEMBL280525 | — | — | 1 | 9.05 |
| CHEMBL285610 | — | — | 1 | 8.96 |
| CHEMBL23308 | — | — | 1 | 8.89 |
| CHEMBL23375 | — | — | 1 | 8.89 |
| CHEMBL432657 | — | — | 1 | 8.82 |
| CHEMBL23123 | — | — | 1 | 8.80 |
| CHEMBL282114 | — | — | 1 | 8.80 |
| CHEMBL282189 | — | — | 1 | 8.74 |
| CHEMBL23572 | — | — | 1 | 8.72 |
| CHEMBL24815 | — | — | 1 | 8.70 |
| CHEMBL26229 | — | — | 1 | 8.68 |
| CHEMBL24543 | — | — | 1 | 8.68 |
| CHEMBL280624 | — | — | 1 | 8.68 |
| CHEMBL279903 | — | — | 1 | 8.66 |
| CHEMBL26102 | — | — | 1 | 8.64 |
| CHEMBL25419 | — | — | 1 | 8.55 |
| CHEMBL26775 | — | — | 1 | 8.55 |
| CHEMBL24587 | — | — | 1 | 8.52 |
| CHEMBL24536 | — | — | 1 | 8.51 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 8.46 |
| CHEMBL23992 | — | — | 1 | 8.41 |
| CHEMBL177716 | — | — | 1 | 8.40 |
| CHEMBL283562 | — | — | 1 | 8.35 |
| CHEMBL25311 | — | — | 1 | 8.30 |
| CHEMBL24653 | — | — | 1 | 8.30 |
| CHEMBL441223 | — | — | 1 | 8.27 |
| CHEMBL281772 | — | — | 1 | 8.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26396 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL282709 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL280525 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL286723 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL285610 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL23308 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL23375 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL432657 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL23123 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL282114 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL282189 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL23572 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL24815 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL24543 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL26229 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL280624 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL279903 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL26102 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL25419 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL26775 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL24587 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL24536 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL23992 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL177716 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL283562 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL24653 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL25311 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL441223 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL281772 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL283242 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL280578 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL280699 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL285573 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL487704 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL281087 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL25985 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL24228 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL26445 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL280576 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL277692 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL280993 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL446663 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL281065 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL23513 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL436144 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL488322 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL24552 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL440786 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL282528 | — | IC50 | = | 130.0 | nM | 6.89 |